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Compound Detail

CHEMBL207236

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CCCc1c(OCCCN(C)c2ccccc2)ccc2c(C(F)(F)F)noc12

Basic Information

ChEMBL ID CHEMBL207236
Phase Preclinical
Structure Type MOL
InChI Key FFEMTQPBRTULCE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

392.4
MW (Da)
5.70
ALogP
4
HBA
0
HBD
38.5
PSA (Ų)
0.46
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23F3N2O2
MW 392.42
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.91

Activity Summary

IC50 2 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-alpha
CHEMBL2808
IC50 6.43 6.43 372.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
IC50 6.37 6.37 428.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxysterols receptor LXR-alpha IC50 = 372.0 nM 6.43 Inhibition of LXR alpha 16529931
Oxysterols receptor LXR-beta IC50 = 428.0 nM 6.37 Inhibition of LXR beta 16529931

Literature References

PubMed DOI Target Context # Activities
16529931 10.1016/j.bmcl.2006.02.050 Oxysterols receptor LXR-alpha 2
16529931 10.1016/j.bmcl.2006.02.050 Oxysterols receptor LXR-beta 2
16529931 10.1016/j.bmcl.2006.02.050 Peroxisome proliferator-activated receptor alpha 1
16529931 10.1016/j.bmcl.2006.02.050 Peroxisome proliferator-activated receptor delta 1
16529931 10.1016/j.bmcl.2006.02.050 Peroxisome proliferator-activated receptor gamma 1

Data from ChEMBL 36 via Core Engine